Improvement of Resveratrol Permeation through Sublingual Mucosa: Chemical Permeation Enhancers versus Spray Drying Technique to Obtain Fast-Disintegrating Sublingual Mini-Tablets

Abstract

Resveratrol (RSV) is a natural polyphenol with several interesting broad-spectrum pharmacological properties. However, it is characterized by poor oral bioavailability, extensive first-pass effect metabolism and low stability. Indeed, RSV could benefit from the advantage of the sublingual route of administration. In this view, RSV attitudes to crossing the porcine sublingual mucosa were evaluated and promoted both by six different chemical permeation enhancers (CPEs) as well as by preparing four innovative fast-disintegrating sublingual mini-tablets by spray drying followed by direct compression. Since RSV by itself exhibits a low permeation aptitude, this could be significantly enhanced by the use of CPEs as well as by embedding RSV in a spray-dried powder to be compressed in order to prepare fast-disintegrating mini-tablets. The most promising observed CPEs (menthol, lysine and urea) were then inserted into the most promising spray-dried excipients’ compositions (RSV-B and RSV-C), thus preparing CPE-loaded mini-tablets. However, this procedure leads to unsatisfactory results which preclude the possibility of merging the two proposed approaches. Finally, the best spray-dried composition (RSV-B) was further evaluated by SEM, FTIR, XRD and disintegration as well as dissolution behavior to prove its effectiveness as a sublingual fast-disintegrating formulation.

Spray-Dried Cytisine-Loaded Matrices: Development of Transbuccal Sustained-Release Tablets as a Promising Tool in Smoking Cessation Therapy

“…CYT-loaded buccal tablets were immediately prepared by compressing the previously freshly prepared spray-dried powders. Carefully weighed amounts of powder (20 mg) were directly compressed (10 tons) by using a hydraulic, single-die tableting machine (Perkin Elmer IR Accessory, Waltham, MA, USA), two flat-faced punches and a die [20]. Tablets of 0.65 cm of diameter were obtained.…”

“…Xylitol is a sugar polyol that could also improve drug permeability, acting as permeation enhancer molecule. Finally, propylene glycol was also chosen as a hydrophilic excipient as it is able to promote buccal permeation and tissue accumulation of active compounds in association with polyols, thus making it indispensable for the preparation of solid buccal formulations [20,37].…”

“…In this work, four powders (S-CYT-A, S-CYT-B, S-CYT-C and S-CYT-D) characterized by different excipient ratios were obtained by spray-drying. The spray-drying method was chosen since it is easily scalable, cost-effective, and valuable to obtain dry pharmaceutical powders that are homogeneous in terms of both particle size (narrow size distribution) and drug loading [20]. This process is characterized by some relevant parameters (e.g., type of solvent, flow rate, inlet temperature, starting solution concentration, spray-dried volume), which directly affect the characteristics of the final spray-dried product.…”

Grapefruit IntegroPectin isolation via spray drying and via freeze drying: a comparison

“…This is in agreement with the higher antioxidant power observed for the spray dried powder, and with the fact that the exposure of the heat-resistant biophenols to the relatively high temperatures of the spray drying process is so brief to not induce their molecular degradation, as previously noted also for resveratrol. [13] 3.4 Total phenol and total protein content. Table 3 shows the outcomes of the Folin-Ciocalteu and Bradford assays alongside the main flavonoid content quantified via HPLC-DAD.…”

Dual Nanostructured Lipid Carriers/Hydrogel System for Delivery of Curcumin for Topical Skin Applications

“…From the amount of CUR penetrated into membranes (Q T ), the amount of drug entrapped per unit area (De) was calculated as follows [ 40 ]: De = Q T /A where A is the area available for penetration (2.54 cm 2 )…”